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Assay Detail

CHEMBL685131

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of [3H]dexamethasone binding to human Glucocorticoid Receptor
4
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

Glucocorticoid receptor (CHEMBL2034)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Selective plasma hydrolysis of glucocorticoid gamma-lactones and cyclic carbonates by the enzyme paraoxonase: an ideal plasma inactivation mechanism.
Biggadike K, Angell RM, Burgess CM, Farrell RM, Hancock AP, Harker AJ, Irving WR, Ioannou C, Procopiou PA, Shaw RE, Solanke YE, Singh OM, Snowden MA, Stubbs RJ, Walton S, Weston HE.
J Med Chem (2000) 43 : 19 -21
PubMed 10633034 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 8.17 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1473 FLUTICASONE PROPIONATE 4.0 1 9.30
CHEMBL302366 2 8.47
CHEMBL63241 1 6.71

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1473 FLUTICASONE PROPIONATE IC50 = 0.5 nM 9.30
CHEMBL302366 IC50 = 3.4 nM 8.47
CHEMBL302366 IC50 = 6.6 nM 8.18
CHEMBL63241 IC50 = 194.0 nM 6.71